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Allosteric Modulation of GPCRs of Class A by Cholesterol
J. Jakubík, EE. El-Fakahany
Jazyk angličtina Země Švýcarsko
Typ dokumentu časopisecké články, přehledy
Grantová podpora
19-05318S
Grantová Agentura České Republiky
RVO:67985823
Akademie Věd České Republiky
Free Medical Journals od 2000
Freely Accessible Science Journals od 2000
PubMed Central od 2007
Europe PubMed Central od 2007
ProQuest Central od 2000-03-01
Open Access Digital Library od 2000-01-01
Open Access Digital Library od 2007-01-01
Health & Medicine (ProQuest) od 2000-03-01
ROAD: Directory of Open Access Scholarly Resources od 2000
Odkazy
PubMed
33669406
DOI
10.3390/ijms22041953
Knihovny.cz E-zdroje
- MeSH
- alosterická regulace MeSH
- anticholesteremika farmakologie terapeutické užití MeSH
- buněčná membrána metabolismus MeSH
- cholesterol chemie metabolismus MeSH
- cílená molekulární terapie metody MeSH
- lidé MeSH
- ligandy MeSH
- receptory spřažené s G-proteiny chemie klasifikace metabolismus MeSH
- vazba proteinů MeSH
- vazebná místa účinky léků MeSH
- zvířata MeSH
- Check Tag
- lidé MeSH
- zvířata MeSH
- Publikační typ
- časopisecké články MeSH
- přehledy MeSH
G-protein coupled receptors (GPCRs) are membrane proteins that convey extracellular signals to the cellular milieu. They represent a target for more than 30% of currently marketed drugs. Here we review the effects of membrane cholesterol on the function of GPCRs of Class A. We review both the specific effects of cholesterol mediated via its direct high-affinity binding to the receptor and non-specific effects mediated by cholesterol-induced changes in the properties of the membrane. Cholesterol binds to many GPCRs at both canonical and non-canonical binding sites. It allosterically affects ligand binding to and activation of GPCRs. Additionally, it changes the oligomerization state of GPCRs. In this review, we consider a perspective of the potential for the development of new therapies that are targeted at manipulating the level of membrane cholesterol or modulating cholesterol binding sites on to GPCRs.
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- $a G-protein coupled receptors (GPCRs) are membrane proteins that convey extracellular signals to the cellular milieu. They represent a target for more than 30% of currently marketed drugs. Here we review the effects of membrane cholesterol on the function of GPCRs of Class A. We review both the specific effects of cholesterol mediated via its direct high-affinity binding to the receptor and non-specific effects mediated by cholesterol-induced changes in the properties of the membrane. Cholesterol binds to many GPCRs at both canonical and non-canonical binding sites. It allosterically affects ligand binding to and activation of GPCRs. Additionally, it changes the oligomerization state of GPCRs. In this review, we consider a perspective of the potential for the development of new therapies that are targeted at manipulating the level of membrane cholesterol or modulating cholesterol binding sites on to GPCRs.
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